In vitro metabolism of obovatol and its effect on cytochrome P450 enzyme activities in human liver microsomes = 오보바톨의 대사 물질 분석 및 안정성
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- In vitro metabolism of obovatol and its effect on cytochrome P450 enzyme activities in human liver microsomes = 오보바톨의 대사 물질 분석 및 안정성
- J Joo; D Lee; Z Wu; J H Shin; H S Lee; Byoung-Mog Kwon; T L Huh; Y W Kim; S J Lee; T W Kim; T Lee; K H Liu
- Bibliographic Citation
- Biopharmaceutics & Drug Disposition, vol. 34, no. 4, pp. 195-202
- Publication Year
- Obovatol, a major constituent of the leaves of Magnolia obovata Thunb, is known to inhibit nuclear factor-κB activity and arachidonic acid-induced platelet aggregation. This study was performed to identify the metabolites of obovatol in human liver microsomes. Human liver microsomes incubated with obovatol in the presence of NADPH and/or UDPGA resulted in the formation of six metabolites, M1-M6. M1 and M2 were identified as hydroxyobovatol, on the basis of liquid chromatography/tandem mass spectrometric (LC-MS/MS) analysis. M1, M2 and obovatol were further metabolized to their glucuronide conjugates, obovatol-glucuronide (M3), obovatol-diglucuronide (M4) and hydroxyobovatol- glucuronide (M5 and M6). The inhibitory potency of obovatol on eight major human P450s was also investigated in human liver microsomes. In these experiments, obovatol strongly inhibited CYP2C19-mediated S-mephenytoin hydroxylase activity with an IC50 value of 0.8 μm, which could have implications for drug-drug interactions.
- glucuronidationmicrosomesdrug interactionobovatoloxidation
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